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Chemical Structure : Omipalisib
CAS No.: 1086062-66-9
Catalog No.: PC-42513Not For Human Use, Lab Use Only.
Omipalisib (GSK2126458) is a highly potent dual inhibitor PI3K/mTOR inhibitor with app Ki of 19/130/24/60/180/300 nM for p110α/p110β/p110γ/p110δ/mTORC1/mTORC2 respectively.
| Packing | Price | Stock | Quantity |
|---|---|---|---|
| 25 mg | $218 | In stock | |
| 100 mg | $498 | In stock | |
| 200 mg | $768 | In stock | |
| 1 g | Get quote |
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Omipalisib (GSK2126458) is a highly potent dual inhibitor PI3K/mTOR inhibitor with app Ki of 19/130/24/60/180/300 nM for p110α/p110β/p110γ/p110δ/mTORC1/mTORC2 respectively.
GSK2126458 shows equivalent activity for p110α mutants E542K/E545K/H1047R with Ki of 8/8/9 nM.
GSK2126458 inhibits pAKT-S473 in T47D cells (IC50=0.41 nM), also inhibits phosphorylation of AKTT308 and p70S6K.
GSK2126458 is active in vivo and orally bioavailable.
| M.Wt | 505.496 | |
| Formula | C25H17F2N5O3S | |
| Appearance | Solid | |
| Storage |
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| Solubility |
10 mM in DMSO |
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| Chemical Name/SMILES |
Benzenesulfonamide, 2,4-difluoro-N-[2-methoxy-5-[4-(4-pyridazinyl)-6-quinolinyl]-3-pyridinyl]- |
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1. Knight SD, et al. ACS Med Chem Lett. 2010 Jan 19;1(1):39-43.
2. Khalili JS, et al. Clin Cancer Res. 2012 Aug 15;18(16):4345-55.
3. Munster P, et al. Clin Cancer Res. 2016 Apr 15;22(8):1932-9.
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